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Synthesis and cercaricidal activities of a serial of novel self-diffused cercaricides derived from niphensamide 被引量：2

Synthesis and cercaricidal activities of a serial of novel self-diffused cercaricides derived from niphensamide
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摘要 A serial of novel cercaricides that can self-diffuse on the water surface were designed and synthesized according to the special habit of cercariae larvae.These compounds were derived from niphensamide.While the compounds were dropped on the surface of water,the liquor diffused along the air-water interface and formed thin membranes floating on the water surface immediately.The strong cercaricidal activities against the cereariae larvae of Schistosome japonicum of these compounds have been revealed by further experiments. A serial of novel cercaricides that can self-diffuse on the water surface were designed and synthesized according to the special habit of cercariae larvae.These compounds were derived from niphensamide.While the compounds were dropped on the surface of water,the liquor diffused along the air-water interface and formed thin membranes floating on the water surface immediately.The strong cercaricidal activities against the cereariae larvae of Schistosome japonicum of these compounds have been revealed by further experiments.
作者 Wei Guo Lv Yin Zheng Yong Quan Wu Xiao Lin Fan
机构地区 Key Laboratory of Organo-pharmaceutical Chemistry of Jiangxi Province
出处 《Chinese Chemical Letters》 SCIE CAS CSCD 2008年第4期406-408,共3页 中国化学快报（英文版）
基金 the financial support from National Natural Science Foundation of China(Nos.50478117,50568001) Supports from the invite public important bidding project of Jiangxi province(2006) science foundation of Jiangxi provincial Department Education(No.GJJ08385)are also acknowledged.
关键词 Niphensamide Self-diffused cercaricide Cercariae larvae Niphensamide Self-diffused cercaricide Cercariae larvae
分类号 TQ453 [化学工程—农药化工]
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参考文献7

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  • 6[6]The data of product 5a:a yellow oil (0.38 g,yield of 80%).IR v(KBr):3510,3321,3079,2874,1677,1601,1552,1507,1335,1269,1219,1109,1040,914,857,818,744,664 cm-1.1H N MR (400 MHz,CDCl3,δ ppm):10.67 (s,1H,H-8),8.20 (d,2H,J=9.2 Hz,H-13,H-11),8.17 (m,1H,H-6),7.94 (d,2H,J=9.2 Hz,H-10,H-14),7.42 (d,1H,J=8.8 Hz,H-2),6.95 (d,1H,J=8.8 Hz,H-3),3.47-4.35 (m,PEG-H),2.42 (s,1H,OH).MS:[M-H]+ m/z (%) 467 (M+-H,n=4),511 (M+-H,n=5);[M+Na]+ m/z (%) 491 (M++Na,n=4),535 (M++Na,n=5).5b:a yellow oil (0.48 g,yield of 85%).IR v(KBr):3509,3321,3078,2874,1678,1600,1551,1508,1336,1270,1220,1110,932,857,816,715,665 cm-1.1H NMR (400 MHz,CDCl3,δ ppm):10.47 (s,1 H,H-8),8.25 (d,2H,J=9.2 Hz,H-13,H-11),8.19 (m,1H,H-6),7.97 (d,2H,J=9.2 Hz,H-10,H-14),7.46 (d,1H,J=8.8 Hz,H-2),6.99 (d,1H,J=8.8 Hz,H-3),3.48-4.38 (m,PEG-H),2.45 (s,1H,OH).MS:[M-HI+ m/z (%),555 (M+-H,n=6),599 (M+-H,n=7);[M+Na]+ m/z (%) 579 (M++Na,n=6),623 (M++Na,n=7).5c:a yellow oil (0.53 g,yield of 78%).IR v(KBr):3511,3320,3068,2874,1678,1599,1551,1508,1336,1270,1219,1109,1040,941,857,816,715,664 cm-1.1H NMR (400 MHz,CDCl3,δ ppm):10.43 (s,1H,H-8),8.22 (d,2H,J=9.2 Hz,H-13,H-11),8.18 (m,1H,H-6),7.96 (d,2H,J=9.2 Hz,H-10,H-14),7.44 (d,1H,J=8.8 Hz,H-2),6.97 (d,1H,J=8.8 Hz,H-3),3.46-4.35 (m,PEG-H),2.42 (s,1H,OH).MS:[M-H]+ m/z (%) 643 (M+-H,n=8),687 (M+-H,n=9),731 (M+-H,n=10);[M+Na]+ m/z (%) 667 (M++Na,n=8),711 (M++Na,n=9),755 (M++Na,n=10).5d:a yellow oil (0.66 g,yield of 75%).IR v(KBr):3512,3320,3076,2872,1678,1599,1551,1508,1336,1269,1108,1040,945,857,716,665 cm-1.IH NMR (400 MHz,CDCl3,δ ppm):10.45 (s,1H,H-8),8.24 (d,2H,J=9.2 Hz,H-13,H-11),8.20 (m,1H,H-6),7.98 (d,2H,J=9.2 Hz,H-10,H-14),7.46 (d,1H,J=8.8 Hz,H-2),6.99 (d,1H,J=8.8 Hz,H-3),3.52-4.37 (m,PEG-H),2.44 (s,1H,OH).MS:[M-H]+ m/z (%) 819 (M+-H,n=12),863 (M+-H,n=13),907 (M+-H,n=14);[M+Na]+ m/z (%) 843 (M++Na,n=12),887 (M++Na,n=13),931 (M++Na,n=14).Se:a yellow oil (0.75 g,yield of 70%).IR v(KBr):3510,3319,2872,1677,1599,1550,1508,1337,1255,1108,1040,947,854,715,660cm-1.1H NMR (400 MHz,CDCl3,δ ppm):10.45 (s,1H,H-8),8.24 (d,2H,J=9.2 Hz,H-13,H-11),8.21 (m,1H,H-6),7.98 (d,2H,J=9.2 Hz,H-10,H-14),7.46 (d,1H,J=8.8 Hz,H-2),6.98 (d,1H,J=8.8 Hz,H-3),3.47-4.73 (m,PEG-H),2.44 (s,1H,OH).MS:[M-H]+ m/z (%) 995 (M+-H,n=16),1039 (M+-H,n=17),1083 (M+-H,n=18),1127 (M+-H,n=19);[M+Na]+ m/z (%) 1019 (M++Na,n=16),1063 (M++Na,n=17),1107 (M++Na,n=18),1151 (M++Na,n=19).
  • 7[7]S.L.Zhou,J.Y.Lin,M.S.Jiang,Schistosomeology,second ed.,Science Press,Beijing,2001,p.146 (in Chinese).

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Chinese Chemical Letters
2008年 第4期

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